1m17

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[[Image:1m17.gif|left|200px]]
[[Image:1m17.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1m17 |SIZE=350|CAPTION= <scene name='initialview01'>1m17</scene>, resolution 2.60&Aring;
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The line below this paragraph, containing "STRUCTURE_1m17", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=AQ4:[6,7-BIS(2-METHOXY-ETHOXY)QUINAZOLINE-4-YL]-(3-ETHYNYLPHENYL)AMINE'>AQ4</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= egfr ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1m17| PDB=1m17 | SCENE= }}
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|RELATEDENTRY=[[1m14|1M14]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1m17 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1m17 OCA], [http://www.ebi.ac.uk/pdbsum/1m17 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1m17 RCSB]</span>
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}}
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'''Epidermal Growth Factor Receptor tyrosine kinase domain with 4-anilinoquinazoline inhibitor erlotinib'''
'''Epidermal Growth Factor Receptor tyrosine kinase domain with 4-anilinoquinazoline inhibitor erlotinib'''
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[[Category: Sliwkowski, M X.]]
[[Category: Sliwkowski, M X.]]
[[Category: Stamos, J.]]
[[Category: Stamos, J.]]
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[[Category: transferase]]
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[[Category: Transferase]]
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[[Category: tyrosine kinase domain]]
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[[Category: Tyrosine kinase domain]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:30:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:09:53 2008''
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Revision as of 21:30, 2 May 2008

Image:1m17.gif

Template:STRUCTURE 1m17

Epidermal Growth Factor Receptor tyrosine kinase domain with 4-anilinoquinazoline inhibitor erlotinib


Overview

The crystal structure of the kinase domain from the epidermal growth factor receptor (EGFRK) including forty amino acids from the carboxyl-terminal tail has been determined to 2.6-A resolution, both with and without an EGFRK-specific inhibitor currently in Phase III clinical trials as an anti-cancer agent, erlotinib (OSI-774, CP-358,774, Tarceva(TM)). The EGFR family members are distinguished from all other known receptor tyrosine kinases in possessing constitutive kinase activity without a phosphorylation event within their kinase domains. Despite its lack of phosphorylation, we find that the EGFRK activation loop adopts a conformation similar to that of the phosphorylated active form of the kinase domain from the insulin receptor. Surprisingly, key residues of a putative dimerization motif lying between the EGFRK domain and carboxyl-terminal substrate docking sites are found in close contact with the kinase domain. Significant intermolecular contacts involving the carboxyl-terminal tail are discussed with respect to receptor oligomerization.

About this Structure

1M17 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor., Stamos J, Sliwkowski MX, Eigenbrot C, J Biol Chem. 2002 Nov 29;277(48):46265-72. Epub 2002 Aug 23. PMID:12196540 Page seeded by OCA on Sat May 3 00:30:30 2008

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